Abstract
The in vivo metabolism of isoprophenamine was examined following oral administration to mice, rabbits and humans. In mice the drug was metabolized to o-chloromandelic acid which was excreted into urine as one of the main metabolites. Mice excreted also a considerable amount of unchanged compound and its basic metabolites. In rabbits and humans, on the other hand, the drug was converted to o-chlorobenzoic acid and o-chlorohippuric acid as acid metabolites and thus the metabolic patterns were resemble each other. The metabolic pathways of the drug and the relationship between metabolism and pharmacological effect are also discussed.